Urinary urgency is the key symptom of overactive bladder (OAB) and often forces patients to modify their lifestyle or daily routine. The impact of OAB on quality of life is significant. Antimuscarinics, an established pharmaceutical treatment for OAB, were originally thought to affect parasympathetic efferents to the bladder; however, there is increasing evidence of an important effect on afferent pathways. Dry mouth and constipation are the most common undesirable events resulting from the use of these agents. Imipramine, a tricyclic antidepressant, is a useful drug for the treatment of OAB, especially when combined with antimuscarinic agents, although this has not been adequately assessed as yet. One result of research in this field is the upcoming introduction of beta-3 agonists in the treatment of OAB. Botulinum toxin, a minimally invasive medical treatment, represents a new era for the treatment of refractory OAB. Despite the fact that this is currently an off-label treatment, it actually represents a widespread alternative method of therapy when conventional medical treatment fails. Pharmacotherapy will continue to play a major role in the treatment of OAB in the future.